ArticleAntimicrobial agents and chemotherapy2010
Activity of the histone deacetylase inhibitor FR235222 on Toxoplasma gondii: inhibition of stage conversion of the parasite cyst form and study of new derivative compounds.
Article in Antimicrobial agents and chemotherapy, 2010. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 34 papers, 1 of them a synthesis that pooled it.
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Who cites it
34 citing papers in PubMed, 1 synthesis or guideline pooled it, 66 citations in OpenAlex.
- Activities of anti-Toxoplasma drugs and compounds against tissue cysts in the last three decades (1987 to 2017), a systematic review.Parasitology research · 2018Pooled it
- Design, synthesis, and anti-Toxoplasma gondii evaluation of β-carboline derivatives.Parasites & vectors · 2025Article
- Article
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- Proteomic identification of aFEMS microbes · 2025Article
- Identification of fungal natural products with potent inhibition inMicrobiology spectrum · 2024Article
- Epigenetic regulation as a therapeutic target in the malaria parasite Plasmodium falciparum.Malaria journal · 2024Review
- TgKDAC4: A Unique Deacetylase ofMicroorganisms · 2023Article
- A positive feedback loop controls Toxoplasma chronic differentiation.Nature microbiology · 2023Article
- Prenyl Transferases Regulate Secretory Protein Sorting and Parasite Morphology inInternational journal of molecular sciences · 2023Article
- Advances towards the completeFaculty reviews · 2023Review
- Theileria annulata histone deacetylase 1 (TaHDAC1) initiates schizont to merozoite stage conversion.Scientific reports · 2022Article
- A Histone Deacetylase (HDAC) Inhibitor with Pleiotropic In Vitro Anti-International journal of molecular sciences · 2022Article
- The determinants regulatingFrontiers in microbiology · 2022Review
- Crossing of the Cystic Barriers ofMolecules (Basel, Switzerland) · 2021Article
- Toxoplasmosis: Current and Emerging Parasite Druggable Targets.Microorganisms · 2021Review
- Promising Drug Targets and Compounds with Anti-Microorganisms · 2021Review
- Macrocyclic Tetramers-Structural Investigation of Peptide-Peptoid Hybrids.Molecules (Basel, Switzerland) · 2021Article
- Epidemiology, Pathophysiology, Diagnosis, and Management of Cerebral Toxoplasmosis.Clinical microbiology reviews · 2021Review
- Nullscript inhibits Cryptosporidium and Toxoplasma growth.International journal for parasitology. Drugs and drug resistance · 2020Article
Corrections and comments
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Authors and funding
7 authors at 4 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Bradyzoite-to-tachyzoite conversion plays a role in the pathogenesis of recrudescence of ocular toxoplasmosis and disease in immunocompromised persons. The currently available medicines are ineffective on cysts and fail to prevent reactivation of latent toxoplasmosis. A previous study showed that the histone deacetylase inhibitor FR235222 has a dramatic effect on tachyzoite growth and induces tachyzoite-to-bradyzoite conversion in vitro. The present study shows that FR235222 can target in vitro-converted cysts and bradyzoites. Moreover, the compound is active on ex vivo T. gondii cysts. Free bradyzoites isolated after lysis of the cell wall did not proliferate in vitro when the cyst was treated with FR235222. The results imply that this compound is able to cross the T. gondii cystic cell wall. Fluorescent labeling shows that the compound impairs the capacity of the bradyzoites to convert without damaging the cyst wall integrity. In vivo inoculation of formerly treated cysts fails to infect mice when these cysts were treated with FR235222. We used our structural knowledge of FR235222 and its target, T. gondii HDAC3, to synthesize new FR235222 derivative compounds. We identified two new molecules that are highly active against tachyzoites. They harbor a better selectivity index that is more suitable for a future in vivo approach. These results identify FR235222 and its derivatives as new lead compounds in the range of therapeutics available for acute and chronic toxoplasmosis.
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